MEK

Inhibitory Selectivity

Catalog No.	Inhibitor Name	MEK	MEK1	MEK1/2	MEK2	MEK5	Other
A10257	Selumetinib		***
A10256	PD0325901	****
A11029	Trametinib		****		****
A10957	U0126-EtOH		*		**		MKK6/p38 MAPK,MKK3/p38 MAPK
A10212	PD184352		**		**
A10705	PD98059		*
A10151	BIX 02189					****	ERK5,TGFβR1
A10089	Pimasertib			*
A10150	BIX 02188					***	ERK5,TGFβR1
A11040	TAK-733		****
A10115	AZD8330						ERK phosphorylation
A11493	Binimetinib	***		***
A14137	SL-327		*		*		AP-1,MKK3/p38 MAPK
A11264	Refametinib		**		**
A12974	GDC-0623		****
A15762	BI-847325		**		***		Aurora B,Aurora C,Aurora A
A11441	Cobimetinib		***
A10704	PD318088
A10453	Honokiol						Akt-phosphorylation
A11247	RO4927350
A13272	RO4987655	****
A14019	RO5126766 (CH5126766)		*				BRAF, CRAF

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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Refametinib

Catalog No. A11264
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MEK 抑制剂

Refametinib是一种有效的，ATP非竞争性和高度选择性的MEK1和MEK2抑制剂，IC50分别为19 nM和47 nM。了解更多

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GDC-0623

Catalog No. A12974
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MEK1 抑制剂

GDC-0623是一种有效的ATP竞争性MEK1抑制剂，Ki为0.13 nM。了解更多

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PD0325901

Catalog No. A10256
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MEK 抑制剂

PD0325901是一种选择性的，非ATP竞争性MEK抑制剂，无细胞试验中IC50为0.33 nM，对ERK1和ERK2磷酸化抑制作用比CI-1040强500倍左右。了解更多

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- Jan Langkabel, .et al. Induction of peri-implantation stage synthetic embryos using reprogramming paradigms in ESCs, bioRxiv, 2021, January 25
- Ryan Clarke, .et al. Sequential Activation of Guide RNAs to Enable Successive CRISPR-Cas9 Activities, Mol Cell, 2021, Jan 21;81(2):226-238.e5 PMID: 33378644
- Tzeng SF, .et al. O-Glycosylation-mediated signaling circuit drives metastatic castration-resistant prostate cancer, FASEB J, 2018, Jun 15:fj201800687 PMID: 29906246
- Fukumoto S, .et al. Synergistic anti-proliferative effects of mTOR and MEK inhibitors in high-grade chondrosarcoma cell line OUMS-27, Acta Histochem, 2018, Feb;120(2):142-150 PMID: 29397960
- Yoshiteru Yano, .et al. Non-neural and cardiac differentiating properties of Tbx6-expressing mouse embryonic stem cells, Regenerative Therapy, 2016, 3 (2016) 1-6
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GDC-0973 (Cobimetinib)

Catalog No. A11441
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MEK1 抑制剂

GDC-0973 (Cobimetinib,RG7420)是一种有效且高度选择性的MEK1抑制剂，IC50为4.2 nM，对MEK1的选择性选择性是对MEK2的100倍以上，并且当针对一组超过100个丝氨酸的抑制剂进行测试时，没有显示出明显的抑制作用。了解更多

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- Yunping Hu, .et al. FGFR1/MAPK-directed brachyury activation drives PD-L1-mediated immune evasion to promote lung cancer progression, Cancer Lett, 2022, Oct 28;547:215867 PMID: 35985510
- Seidel D, .et al. A multidimensional impedance platform for the real-time analysis of single and combination drug pharmacology in patient-derived viable melanoma models, Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332
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BI-847325

Catalog No. A15762
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MEK/Aurora 抑制剂

BI-847325是一种生物利用型选择性MEK/Aurora双重激酶抑制剂，对于非洲爪蟾Aurora B，人Aurora A和Aurora C以及IC50分别为3 nM，25 nM，15 nM，25 nM和4 nM IC50人MEK1和MEK2。了解更多

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- Hilda Samimi, .et al. Alginate-based 3D cell culture technique to evaluate the half-maximal inhibitory concentration: an in vitro model of anticancer drug study for anaplastic thyroid carcinoma, Thyroid Res, 2021, Dec 3;14(1):27 PMID: 34861882
- Hilda Samimi, .et al. Transcript-level regulation of MALAT1-mediated cell cycle and apoptosis genes using dual MEK/Aurora kinase inhibitor "BI-847325" on anaplastic thyroid carcinoma, DARU J Pharm Sci, 2019, 1-7 PMID: 31077090
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Refametinib (RDEA-119, BAY 86-9766)

Catalog No. A12866
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MEK1/2 抑制剂

Refametinib (RDEA-119,BAY 86-9766)是一种口服生物利用型选择性MEK抑制剂，EC50为 2.0-15 nM。具有潜在的抗肿瘤活性。了解更多

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- Estelle Daudigeos-Dubus, etc. Regorafenib: Antitumor Activity upon Mono and Combination Therapy in Preclinical Pediatric Malignancy Models. PLoS One. 2015; 10(11): e0142612.
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Cobimetinib (racemate)

Catalog No. A15050
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MEK 抑制剂

Cobimetinib (racemate)是一种有效的，高度选择性的MEK1/2抑制剂。了解更多

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- Yuki Shimizu, .et al. Acquired resistance to BRAF inhibitors is mediated by BRAF splicing variants in BRAF V600E mutation-positive colorectal neuroendocrine carcinoma, Cancer Lett, 2022, Sep 1;543 PMID: 35724767
- Chun-Yu Liu, .et al. Varlitinib Downregulates HER/ERK Signaling and Induces Apoptosis in Triple Negative Breast Cancer Cells, Cancers (Basel), 2019, Jan 17;11(1) PMID: 30658422
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PD 198306

Catalog No. A16032
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MEK 抑制剂

PD 198306是一种有效的，选择性的和非ATP竞争性MAPK/ERK激酶（MEK）抑制剂。了解更多

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AZD6244 (Selumetinib)

Catalog No. A10257
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MEK 抑制剂

Selumetinib (AZD6244)是一种有效，高选择性的MEK抑制剂，ARRY142886，AZD-6244和ARRY-142886是MEK 1/2抑制剂，GI50值在14至50 nm之间。了解更多

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- Chia-Chi Chang, .et al. Upregulation of lactate dehydrogenase a by 14-3-3ζ leads to increased glycolysis critical for breast cancer initiation and progression, Oncotarget, 2016, Jun 7; 7(23): 35270-35283 PMID: 27150057
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GSK1120212 (JTP-74057, Trametinib)

Catalog No. A11029
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MEK 抑制剂

GSK1120212 (JTP-74057,Trametinib)强烈阻止了MEK1和MEK2激酶的活性，而不是其他98种激酶的活性。了解更多

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- Nao Yamagishi, .et al. Non-canonical Regulation of EGFR by the Air Pollutant 9,10-Phenanthrenequinone, Biol Pharm Bull, 2022, 45(10):1553-1558 PMID: 36184515
- Hayato Mizuta, .et al. Gilteritinib overcomes lorlatinib resistance in ALK-rearranged cancer, Nat Commun, 2021, Feb 24;12(1):1261 PMID: 33627640
- Keisuke Yanagida, .et al. Sphingosine 1-Phosphate Receptor Signaling Establishes AP-1 Gradients to Allow for Retinal Endothelial Cell Specialization, Dev Cell, 2020, 52 (6), 779-793 PMID: 32059774
- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Kanemaru Y, .et al. Dramatic response of BRAF V600E-mutant epithelioid glioblastoma to combination therapy with BRAF and MEK inhibitor: establishment and xenograft of a cell line to predict clinical efficacy, Acta Neuropathol Commun, 2019, Jul 25;7(1):119 PMID: 31345255
- Chul Min Park, .et al. Mechanisms for DNA-damaging agent-induced inactivation of ErbB2 and ErbB3 via the ERK and p38 signaling pathways, Oncol Lett, 2018, Feb; 15(2): 1758-1762 PMID: 29434871
- Sumi T, .et al. Trametinib downregulates survivin expression in RB1-positive KRAS-mutant lung adenocarcinoma cells, Biochem Biophys Res Commun, 2018, Jun 18;501(1):253-258 PMID: 29727601
- Toshiyuki Sumi, .et al. Survivin knockdown induces senescence in TTF-1-expressing, KRAS-mutant lung adenocarcinomas, Int J Oncol, 2018, Jul; 53(1): 33-46 PMID: 29658609
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Yuki Kawasaki, .et al. Feedback control of ErbB2 via ERK-mediated phosphorylation of a conserved threonine in the juxtamembrane domain, Sci Rep, 2016, 6: 31502 PMID: 27531070
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MEK162 (ARRY-438162, Binimetinib)

Catalog No. A11493
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MEK1/2 抑制剂

MEK162 (ARRY-438162,Binimetinib)是MEK1/2的一种强效、选择性ATP非竞争性抑制剂。了解更多

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- S Shahab, .et al. MEK Inhibition Suppresses Growth of Atypical Teratoid/Rhabdoid Tumors, J Neuropathol Exp Neurol, 2020, Jul 1;79(7):746-753
- Seidel D, .et al. A multidimensional impedance platform for the real-time analysis of single and combination drug pharmacology in patient-derived viable melanoma models, Biosens Bioelectron, 2019, Jan 1;123:185-194 PMID: 30201332
- Alquezar C, .et al. Increasing progranulin levels and blockade of the ERK1/2 pathway: Upstream and downstream strategies for the treatment of progranulin deficient frontotemporal dementia, Eur Neuropsychopharmacol, 2015, Mar;25(3):386-403 PMID: 25624003
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SL-327

Catalog No. A14137
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MKK/MEK 抑制剂

SL-327是MEK1和MEK2的选择性抑制剂（IC50值分别为0.18和0.22μM）；在体外阻断海马LTP。全身性给药后，体内的脑渗透剂会阻止大鼠的恐惧条件和学习，并在小鼠中产生神经保护作用。了解更多

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G-479

Catalog No. A14380
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MEK 抑制剂

G-479是有效的MEK抑制剂。在许多方面，极性分布在整个分子中的G-479被证明具有比GDC-0623更高的生物活性。了解更多

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U0126-EtOH

Catalog No. A10957
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MEK 抑制剂

U0126-EtOH是MEK1和MEK2的抑制剂，IC50分别为72 nM和58 nM。了解更多

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- Hanna Galganska, .et al. Carbon dioxide inhibits COVID-19-type proinflammatory responses through extracellular signal-regulated kinases 1 and 2, novel carbon dioxide sensors, Cell Mol Life Sci, 2021, Dec;78(24):8229-8242 PMID: 34741187
- Paul Mark Medina, .et al. Revealing the anticancer potential of candidate drugs in vivo using Caenorhabditis elegans mutant strains, Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
- Byungki Jang, .et al. The Peptidylarginine Deiminase Inhibitor Cl-Amidine Suppresses Inducible Nitric Oxide Synthase Expression in Dendritic Cells, Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
- Choe YJ, .et al. Nutlin-3 induces HO-1 expression by activating JNK in a transcription-independent manner of p53., Int J Oncol., 2014, 44(3):761-8. PMID: 24366007
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Cobimetinib (R-enantiomer)

Catalog No. A15051
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MEK 抑制剂

Cobimetinib R-enantiomer是Cobimetinib的R对映异构体，Cobimetinib是一种有力的，高选择性的促分裂原活化蛋白激酶（MEK1/2）抑制剂。了解更多

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PD 334581

Catalog No. A16044
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MEK1 抑制剂

PD 334581在生物学研究中用于评估卤素键合，作为合理药物设计的新型相互作用。它也是MEK1的抑制剂。了解更多

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PD98059

Catalog No. A10705
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MEK 抑制剂

PD98059是一种非ATP竞争性的MEK抑制剂，无细胞试验中IC50为2 μM，特异性抑制MEK-1介导的MAPK激活；不直接抑制ERK1或ERK2。了解更多

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- Anna Nakanishi, .et al. Effects of human induced pluripotent stem cell-derived intestinal organoids on colitis-model mice, Regen Ther, 2022, Sep 9;21:351-361 PMID: 36161099
- Isamu Ogawa, .et al. Suspension culture of human induced pluripotent stem cell-derived intestinal organoids using natural polysaccharides, Biomaterials, 2022, Sep;288:121696 PMID: 36038421
- Hanna Galganska, .et al. Carbon dioxide inhibits COVID-19-type proinflammatory responses through extracellular signal-regulated kinases 1 and 2, novel carbon dioxide sensors, Cell Mol Life Sci, 2021, Dec;78(24):8229-8242 PMID: 34741187
- Akinobu Nakamura, .et al. Engineering Orthogonal, Plasma Membrane-Specific SLIPT Systems for Multiplexed Chemical Control of Signaling Pathways in Living Single Cells, ACS Chem Biol, 2020, Apr 17;15(4):1004-1015 PMID: 32162909
- Yang PM, .et al. p38α/S1P/SREBP2 activation by the SAM-competitive EZH2 inhibitor GSK343 limits its anticancer activity but creates a druggable vulnerability in hepatocellular carcinoma, Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
- Kwang Woon Kim, .et al. Dual-Targeting AKT2 and ERK in cancer stem-like cells in neuroblastoma, Oncotarget, 2019, Sep 24; 10(54): 5645-5659 PMID: 31608140
- Tsai CC, .et al. Protease-activated receptor 2 induces migration and promotes Slug-mediated epithelial-mesenchymal transition in lung adenocarcinoma cells, Biochim Biophys Acta Mol Cell Res, 2018, Oct 13. pii: S0167-4889(18)30452-X PMID: 30321617
- Kim MH, .et al. C16?ceramide and sphingosine 1?phosphate/S1PR2 have opposite effects on cell growth through mTOR signaling pathway regulation, Oncol Rep, 2018, Nov;40(5):2977-2987 PMID: 30226616
- Onozato D, .et al. Efficient Generation of Cynomolgus Monkey Induced Pluripotent Stem Cell-Derived Intestinal Organoids with Pharmacokinetic Functions, Stem Cells Dev, 2018, Aug 1;27(15):1033-1045 PMID: 29742964
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RO4927350

Catalog No. A11247
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MEK1/2 抑制剂

RO4927350是一种有效且高度选择性的非ATP竞争性MEK1/2抑制剂。了解更多

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AS703026 (Pimasertib)

Catalog No. A10089
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MEK1/2 抑制剂

AS703026 (Pimasertib)是一种新型的，选择性的，口服可生物利用的MEK1/2抑制剂，可抑制MM细胞的生长和存活以及细胞因子诱导的破骨细胞分化。了解更多

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RO4987655

Catalog No. A13272
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MEK1 抑制剂

RO4987655是一种口服活性小分子，靶向有丝分裂原激活的蛋白激酶激酶1（MAP2K1或MEK1），抑制 MEK1/MEK2，IC50 为 5.2 nM。具有潜在的抗肿瘤活性。了解更多

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PD184352 (CI-1040)

Catalog No. A10212
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MEK1/2 抑制剂

PD184352 (CI-1040)是一种ATP非竞争性MEK1/2抑制剂，在基于细胞的测定中，IC50为17 nM，对MEK1/2的选择性是对MEK5的100倍。了解更多

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- Sachio Suzuki, .et al. A chemogenetic platform for controlling plasma membrane signaling and synthetic signal oscillation, Cell Chem Biol, 2022, Sep 15;29(9):1446-1464 PMID: 35835118
- Masaru Yoshikawa, .et al. Synthetic Protein Condensates That Inducibly Recruit and Release Protein Activity in Living Cells, J Am Chem Soc, 2021, May 5;143(17):6434-6446 PMID: 33890764
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AZD8330

Catalog No. A10115
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MEK 抑制剂

AZD8330是新型，选择性，非ATP竞争性MEK 1/2抑制剂，IC50为7 nM。阶段1。了解更多

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PD318088

Catalog No. A10704
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MEK 抑制剂

PD318088是MEK1和MEK2的抑制剂。了解更多

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RO5126766 (CH5126766)

Catalog No. A14019
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Raf/MEK dual 抑制剂

RO5126766 (CH5126766)是对Raf和MEK丝裂原激活的蛋白激酶（MAPK）具有特异性的蛋白激酶抑制剂，具有潜在的抗肿瘤活性。了解更多

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- Yuki Shimizu, .et al. Acquired resistance to BRAF inhibitors is mediated by BRAF splicing variants in BRAF V600E mutation-positive colorectal neuroendocrine carcinoma, Cancer Lett, 2022, Sep 1;543 PMID: 35724767
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TAK-733

Catalog No. A11040
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MEK 抑制剂

TAK-733是一种有效的，选择性的MEK变构抑制剂，作用于MEK1，IC50为3.2 nM，抑制Abl1，AKT3，c-RAF，CamK1，CDK2及c-Met等活性。了解更多

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